Bropirimine (Synonyms: U-54461; U-54461S; PNU-54461)

Name: Bropirimine
Brand: MedChemExpress
SKU: HY-W008634
Rating: 5.0 (2 reviews)

Cat. No.: HY-W008634 Purity: 99.94%: Data Sheet
COA

SDS
Handling Instructions
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Bropirimine (U-54461; U-54461S; PNU-54461) is an orally active TLR7 agonist. Bropirimine inhibits RANKL-induced osteoclast differentiation of mouse bone marrow-derived macrophages (BMMs). Bropirimine exhibits dose-dependent direct inhibitory effects on colony formation of cultured KK-47 and 724 cells. Bropirimine can be used for the study of cancers and bone metabolic disorders such as osteoporosis.

For research use only. We do not sell to patients.

Bropirimine Chemical Structure

CAS No. : 56741-95-8

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
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25 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Bropirimine

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

TLR7

In Vitro

Bropirimine (0.3-30 μg/mL, 3 d) inhibits RANKL-induced osteoclast differentiation of mouse BMMs in a concentration-dependent manner^[1].
Bropirimine (0.3-30 μg/mL, 3 d) suppresses the formation of resorption pits on dentin disks in mouse BMM cultures with RANKL and M-CSF, and significantly reduces mRNA expression of TRAP and NFATc1^[1].
Bropirimine (1-30 μg/mL, 4 d) inhibits 1α,25(OH)2D3-induced osteoclast differentiation of mouse BMCs in co-cultures with mouse osteoblastic UAMS-32 cells in a concentration-dependent manner^[1].
Bropirimine (1-30 μg/mL, 48 h) significantly suppresses 1α,25(OH)2D3-induced RANKL mRNA expression in mouse osteoblastic UAMS-32 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bropirimine (100-2000 mg/kg, p.o., once daily, 5 consecutive days, starting on day 1 post-tumor inoculation) demonstrates significant anti-tumor efficacy against murine renal-cell carcinoma (Renca) in euthymic BALB/c mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Renca cells (5 × 10⁶) were implanted under the capsule of the left kidney via flank incision into 8-10-week-old female euthymic BALB/c mice^[3]
Dosage:	100, 500, 1000, 2000 mg/kg
Administration:	p.o., once daily, 5 consecutive days, starting on day 1 post-tumor inoculation
Result:	Achieved tumor growth inhibition at the dose of 1000 and 2000 mg/kg.

Molecular Weight

266.10

Formula

C₁₀H₈BrN₃O

CAS No.

56741-95-8

Appearance

Solid

Color

White to off-white

SMILES

O=C1NC(N)=NC(C2=CC=CC=C2)=C1Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (187.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.7580 mL	18.7899 mL	37.5799 mL
5 mM	0.7516 mL	3.7580 mL	7.5160 mL
10 mM	0.3758 mL	1.8790 mL	3.7580 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (276 KB) SDS (418 KB)

COA (250 KB) HNMR (274 KB) RP-HPLC (246 KB) MS (73 KB)

Handling Instructions (2659 KB)

References

[1]. Suzuki H, et al. Bropirimine inhibits osteoclast differentiation through production of interferon-β. Biochem Biophys Res Commun. 2015;467(1):146‐151. [Content Brief]

[2]. Tei Y, et al. In vitro antitumor activity of bropirimine against urinary bladder tumor cells. Anticancer Res. 2002 May-Jun;22(3):1667-71. [Content Brief]

[3]. Fujioka T, et al. Antitumor effects of oral administration of an interferon-inducing pyrimidinone, Bropirimine, on murine renal-cell carcinoma. Cancer Chemother Pharmacol. 1995;36(1):7-12. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.7580 mL	18.7899 mL	37.5799 mL	93.9496 mL
	5 mM	0.7516 mL	3.7580 mL	7.5160 mL	18.7899 mL
	10 mM	0.3758 mL	1.8790 mL	3.7580 mL	9.3950 mL
	15 mM	0.2505 mL	1.2527 mL	2.5053 mL	6.2633 mL
	20 mM	0.1879 mL	0.9395 mL	1.8790 mL	4.6975 mL
	25 mM	0.1503 mL	0.7516 mL	1.5032 mL	3.7580 mL
	30 mM	0.1253 mL	0.6263 mL	1.2527 mL	3.1317 mL
	40 mM	0.0939 mL	0.4697 mL	0.9395 mL	2.3487 mL
	50 mM	0.0752 mL	0.3758 mL	0.7516 mL	1.8790 mL
	60 mM	0.0626 mL	0.3132 mL	0.6263 mL	1.5658 mL
	80 mM	0.0470 mL	0.2349 mL	0.4697 mL	1.1744 mL
	100 mM	0.0376 mL	0.1879 mL	0.3758 mL	0.9395 mL

Bropirimine Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Bropirimine (Synonyms: U-54461; U-54461S; PNU-54461)

Customer Review

Bropirimine Related Antibodies

2 Publications Citing Use of MCE Bropirimine

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Toll-like Receptor (TLR) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Bropirimine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Bropirimine Related Classifications

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Customer Review

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